1-[18F]氟代乙基-L-色氨酸的半自动化合成

doi:10.7538/tws.2010.23.02.0086

同位素 ›› 2010, Vol. 23 ›› Issue (2): 86-92.DOI: 10.7538/tws.2010.23.02.0086

• 放射性药物和标记化合物 • 上一篇下一篇

1-[¹⁸F]氟代乙基-L-色氨酸的半自动化合成

孙婷¹;王世真¹; 唐刚华²; 李兆陇³

1．中国医学科学院北京协和医学院，北京协和医院核医学科，北京100730;2. 中山大学附属第一医院核医学科，广东广州510080；3 清华大学化学系，北京100084

收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2010-05-20 发布日期:2010-05-20

Semi-automated Synthesis of 1-[¹⁸F]fluoroethyl-L-tryptophan

SUN Ting¹; WANG Shih-Chen¹; TANG Gang-hua²; LI Zhao-long³

1. Department of Nuclear Medicine, PUMC Hospital， Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100730, China; 2. Department of Nuclear Medicine, the Frist Aflliated Hospital, Sun Yai-Sen University, Guangzhou 510080, China; 3.Department of Chemistry, Tsinghua University, Beijing 100084, China

Received:1900-01-01 Revised:1900-01-01 Online:2010-05-20 Published:2010-05-20

摘要/Abstract

摘要： 设计并合成了一种新型氟标记氨基酸类似物1-[¹⁸F]氟代乙基-L-色氨酸（1-[¹⁸F]FETrp）。以色氨酸为原料，采用有机合成法经过七步反应，合成了标准品1-[¹⁹F]FETrp；使用氟多功能模块，采用亲核取代法，将放射化学标记自动化。经过对1-[¹⁹F]FETrp自动化合成条件的摸索，最后采用二锅法合成了1-[¹⁸F]FETrp。1-[¹⁸F]FETrp的放化产率为1.5%，合成时间50 min；由于放化产率过低，今后需改变条件或者寻找新的合成路线以提高产率，以期为临床区分炎症和肿瘤提供新的PET显像剂。

关键词: 1-[¹⁸F]氟代乙基-L-色氨酸（1-[¹⁸F]FETrp）, PET显像剂, 半自动化合成

Abstract: A novel [¹⁸F]fluoro amnio acid analogue 1-[¹⁸F]fluoroethyl -L- tryptophan (1-[¹⁸F]FETrp) was designed and synthesized. The cold standard 1-[¹⁹F]FETrp was synthesized by sevenstep reactions, starting from tryptophan. Then fluoromultifunctional chemistry process control unit (CPCU) was used to synthesize 1-[¹⁹F]FETrp by nucleophilic fluorination. 1-[¹⁸F]FETrp was synthesized in a twostep semiautomated procedure. The no decay corrected radiochemica1 yield of 1-[¹⁸F]FETrp was 1.5％ within 50 min total reaction time. Further experimental work is needed to improve the radiochemical yield, with the hope of attaining a satisfacting new PET imaging agent for differentiating the tumors and inflammation.

Key words:

1-[¹⁸F]fluoroethyl-L-tryptophan (1-[¹⁸F]FETrp), PET imaging agent, semi-automated synthesis

孙婷 ;王世真 ; 唐刚华 ; 李兆陇 . 1-[¹⁸F]氟代乙基-L-色氨酸的半自动化合成[J]. 同位素, 2010, 23(2): 86-92.

SUN Ting; WANG Shih-Chen; TANG Gang-hua; LI Zhao-long. Semi-automated Synthesis of 1-[¹⁸F]fluoroethyl-L-tryptophan[J]. Journal of Isotopes, 2010, 23(2): 86-92.

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1-[¹⁸F]氟代乙基-L-色氨酸的半自动化合成

Semi-automated Synthesis of 1-[¹⁸F]fluoroethyl-L-tryptophan

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